Third-generation inhibitors targeting EGFR T790M mutation in advanced non-small cell lung cancer.

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Wang S, Cang S, Liu D

Third-generation inhibitors targeting EGFR T790M mutation in advanced non-small cell lung cancer.

J Hematol Oncol. 2016 Apr 12;9:34. doi: 10.1186/s13045-016-0268-z.

PubMed ID
27071706 [ View in PubMed
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Abstract

The tyrosine kinase inhibitors (TKI) against epidermal growth factor receptor (EGFR) are widely used in patients with non-small cell lung cancer (NSCLC). However, EGFR T790M mutation leads to resistance to most clinically available EGFR TKIs. Third-generation EGFR TKIs against the T790M mutation have been in active clinical development. These agents include osimertinib, rociletinib, HM61713, ASP8273, EGF816, and PF-06747775. Osimertinib and rociletinib have shown clinical efficacy in phase I/II trials in patients who had acquired resistance to first- or second-generation TKIs. Osimertinib (AZD9291, TAGRISSO) was recently approved by FDA for metastatic EGFR T790M mutation-positive NSCLC. HM61713, ASP8237, EGF816, and PF-06747775 are still in early clinical development. This article reviews the emerging data regarding third-generation agents against EGFR T790M mutation in the treatment of patients with advanced NSCLC.

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